Repro_Pharm Flashcards

(64 cards)

1
Q

Leuprolide- MOA?

A

GnRH analog w/ agonist properties when used in pulsatile fashion
- antagonist properties when used in continuous fashion (downregulates GnRH receptor in pituitary –> dec’d FSH/LH)

“LEUprolide can be used in LIEU of GnRH”

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2
Q

Leuprolide- Clinical uses?

A
  • Infertility (pulsatile)
  • Prostate cancer (continuous w/ Flutamide)
  • Uterine fibroids (continuous)
  • Precocious puberty (continuous)
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3
Q

Leuprolide- Toxicity?

A
  • Anti-androgen
  • Nausea
  • Vomiting
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4
Q

Testosterone- MOA?

A

Agonist @ androgen receptors

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5
Q

Testosterone- Clinical uses?

A
  • Treats hypogonadism & promotes development of secondary sex characteristics
  • Stimulation of anabolism to promote recovery after burn or injury
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6
Q

Testosterone- Toxicity?

A
  • Causes masculinization in females
  • Reduces intratesticular testosterone in males by inhibiting release of LH (via negative feedback), leading to gonadal atrophy
  • Premature closure of epiphyseal plates
  • Inc’d LDL, dec’d HDL
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7
Q

Methyltestosterone- MOA?

A

Agonist @ androgen receptors

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8
Q

Methyltestosterone- Clinical uses?

A
  • Treats hypogonadism & promotes development of secondary sex characteristics
  • Stimulation of anabolism to promote recovery after burn or injury
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9
Q

Methyltestosterone- Toxicity?

A
  • Causes masculinization in females
  • Reduces intratesticular testosterone in males by inhibiting release of LH (via negative feedback), leading to gonadal atrophy
  • Premature closure of epiphyseal plates
  • Inc’d LDL, dec’d HDL
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10
Q

5-alpha-reductase: function?

A

Converts Testosterone –> DHT (more potent)

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11
Q

Finasteride- MOA?

A

5-alpha-reductase inhibitor (dec’d conversion of Testosterone to DHT)

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12
Q

Finasteride- Clinical uses?

A
  • BPH
  • Promotes hair growth – used to treat male-pattern baldness

(to prevent male-pattern baldness, give a drug that will encourage female breast growth)

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13
Q

Flutamide- MOA?

A

A non-steroidal competitive inhibitor of androgens @ the Testosterone receptor

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14
Q

Flutamide- Clinical uses?

A

Prostate Carcinoma

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15
Q

Ketoconazole- MOA?

A

Inhibits steroid synthesis (inhibitrs 17,20-desmolase)

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16
Q

Ketoconazole- Clinical uses?

A

Polycystic Ovarian Syndrome (to prevent hirsutism)

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17
Q

Ketoconazole- Side effects?

A

Gynecomastia & amenorrhea

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18
Q

Spironolactone- MOA?

A

Inhibits steroid binding

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19
Q

Spironolactone- Clinical uses?

A

Polycystic Ovarian Syndrome (to prevent hirsutism)

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20
Q

Spironolactone- Side effects?

A

Gynecomastia & amenorrhea

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21
Q

Ethinyl Estradiol- MOA?

A

(Estrogen)

Binds estrogen receptors

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22
Q

Ethinyl Estradiol- Clinical uses?

A

Women:

  • Hypogonadism or ovarian failure
  • Menstrual abnormalities
  • HRT in postmenopausal women

Men:
- Androgen-dependent prostate cancer

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23
Q

Ethinyl Estradiol- Toxicity?

A
  • Inc’d risk of endometrial cancer
  • Bleeding in postmenopausal women
  • Inc’d risk of thrombi
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24
Q

Ethinyl Estradiol- Contraindications?

A
  • ER-positive breast cancer

- History of DVTs

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25
DES- MOA?
(Estrogen) | Binds estrogen receptors
26
DES- Clinical uses?
Women: - Hypogonadism or ovarian failure - Menstrual abnormalities - HRT in postmenopausal women Men: - Androgen-dependent prostate cancer
27
DES- Toxicity?
- Inc'd risk of endometrial cancer - Bleeding in postmenopausal women - Clear cell adenocarcinoma of vagina if exposed in-utero - Inc'd risk of thrombi
28
DES- Contraindications?
- ER-positive breast cancer | - History of DVTs
29
Mestranol- MOA?
(Estrogen) | Binds estrogen receptors
30
Mestranol- Clinical uses?
Women: - Hypogonadism or ovarian failure - Menstrual abnormalities - HRT in postmenopausal women Men: - Androgen-dependent prostate cancer
31
Mestranol- Toxicity?
- Inc'd risk of endometrial cancer - Bleeding in postmenopausal women - Inc'd risk of thrombi
32
Mestranol- Contraindications?
- ER-positive breast cancer | - History of DVTs
33
Clomiphene- MOA?
Selective Estrogen Receptor Modulator (SERM) - Partial agonist @ estrogen receptors in hypothalamus - Prevents normal feedback inhibition & increases release of LH & FSH from pituitary, which stimulates ovulation
34
Clomiphene- Clinical uses?
- Infertility | - Polycystic Ovarian Syndrome
35
Clomiphene- Adverse effects?
- Hot flashes - Ovarian enlargement - Multiple, simultaneous pregnancies - Visual disturbances
36
Tamoxifen- MOA?
Selective Estrogen Receptor Modulator (SERM) - Antagonist on breast tissue
37
Tamoxifen- Clinical uses?
Used to treat & prevent recurrence of ER-positive breast cancer
38
Raloxifene- MOA?
Selective Estrogen Receptor Modulator (SERM) - Agonist on bone, CV system, & blood lipoproteins (reduces resorption of bone) - Antagonist in breast & uterus
39
Raloxifene- Clinical uses?
Used to treat Osteoporosis | also decreases risk of both breast & uterine cancer
40
Hormone Replacement Therapy -- a) What is it used for? b) What are its components? c) Potential AEs?
a) Used for relief or prevention of menopausal symptoms (e.g. hot flashes, vaginal atrophy) & osteoporosis ( ↑estrogen, ↓osteoclast activity) b) Unopposed estrogen replacement therapy (ERT) ↑the risk of endometrial cancer, so progesterone is added c) Possible ↑CV risk
41
Anastrozole - MOA?
Aromatase inhibitor
42
Anastrozole - Clinical uses?
Used in postmenopausal women w/ breast cancer
43
Exemestane - MOA?
Aromatase inhibitor
44
Exemestane - Clinical uses?
Used in postmenopausal women w/ breast cancer
45
Progestins - MOA?
Bind progesterone receptors, reduce growth & ↑ vascularization of endometrium
46
Progestins - Clinical uses?
- Oral contraceptives | - Tx of endometrial cancer & abnormal uterine bleeding
47
Mifepristone (RU-486) - MOA?
Competitive inhibitor of progestins @ progesterone receptor
48
Mifepristone - Clinical uses?
Termination of pregnancy -- Administered w/ Misoprostol (PGE1)
49
Mifepristone - Toxicity?
- Heavy bleeding - GI effects (nausea, vomiting, anorexia) - Abdominal pain
50
Terbutaline - MOA?
B2-agonist that relaxes the uterus
51
Terbutaline - Clinical uses?
Reduces premature uterine contractions
52
Tamsulosin - MOA?
α-1 antagonist | - selective for α-1A,D receptors (found on prostate) & vascular α-1B receptors
53
Tamsulosin- Clinical uses?
Used to treat BPH by inhibiting smooth muscle contraction
54
Sildenafil - MOA?
Inhibits phosphodiesterase 5, causing ↑cGMP, smooth muscle relaxation in the corpus cavernous, ↑blood flow, & penile erection
55
Sildenafil - Clinical uses?
Treatment of erectile dysfunction
56
Vardenafil - MOA?
Inhibits phosphodiesterase 5, causing ↑cGMP, smooth muscle relaxation in the corpus cavernous, ↑blood flow, & penile erection
57
Vardenafil - Clinical uses?
Treatment of erectile dysfunction
58
Sildenafil - Toxicity?
- Headache - Flushing - Dyspepsia - Impaired blue-green color vision - Risk of life-threatening hypotension in patients taking nitrates " Hot & Sweaty," but then Headache, Heartburn, & Hypotension
59
Vardenafil - Toxicity?
- Headache - Flushing - Dyspepsia - Impaired blue-green color vision - Risk of life-threatening hypotension in patients taking nitrates " Hot & Sweaty," but then Headache, Heartburn, & Hypotension
60
Danazol - MOA?
Synthetic androgen that acts as a partial agonist @ androgen receptors
61
Danazol - Clinical uses?
Endometriosis & hereditary angioedema
62
Danazol - Toxicity?
- Weight gain - Edema - Acne - Hirsutism - Masculinization - ↓HDL levels - Hepatotoxicity
63
Medroxyprogesterone - Clinical uses?
- Reduces the incidence of endometrial hyperplasia & the risk of endometrial carcinoma in postmenopausal women on estrogen replacement therapy - Also used parentally as long-acting contraceptive
64
Medroxyprogesterone - AEs of prolonged use?
Decreased bone mineral density in women of all ages